IP Library Granted Patent US 10,550,089
Granted Patent B2
US 10,550,089 · App. 16/300,641 · Granted Feb 4, 2020

Inhibitors of protease-activated receptor-2

Inventors: John Graham Cumming (Basel, CH); Frank Xinhe Wu (Waltham, MA); Karl Henrik Edman (Mölndal, SE); Hongming Chen (Mölndal, SE); Dean Gordon Brown (Waltham, MA); Roland Werner Burli (Cambridge, GB); Shawn Donald Johnstone (Saint Laurent, CA); Giles Albert Brown (Cambridge, GB); Benjamin Gerald Tehan (Cambridge, GB); Barry John Teobald (Cambridge, GB); Miles Stuart Congreve (Cambridge, GB)
Assignee: Heptares Therapeutics Limited
C07D233/64A61P17/00A61P29/00C07D249/08C07D403/06C07D403/10C07D405/06C07D409/06C07D413/10C07D417/10C07D471/04A61K31/4164
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Quick Facts
Patent No.
US 10,550,089
App. No.
16/300,641
Granted
Feb 4, 2020
Kind
B2
Abstract

The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R 1 -R 3 are as defined herein.

Claims (10)

1. A compound which is selected from the group consisting of:

and

pharmaceutically acceptable salts thereof.

2. A pharmaceutical composition comprising (a) a compound of claim 1 and (b) a pharmaceutically acceptable excipient.

3. A method of treating a disease or disorder mediated by PAR2 activity, comprising administering to a subject in need of such treatment an effective amount of at least one compound of claim 1 .

4. The method of claim 3 , wherein the disease or disorder is pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, or colitis.

5. A method of modulating the activity of PAR2, comprising contacting a cell comprising the PAR2 with an effective amount of at least one compound of claim 1 .

6. A method of treating a disease or disorder in a patient in need thereof, comprising administering a compound of claim 1 , wherein the disease or disorder is pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, or colitis.

7. The compound of claim 1 , wherein the compound is selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

Assignments (3)
CHANGE OF NAME Recorded Jun 7, 2024
From: HEPTARES THERAPEUTICS LIMITED
To: NXERA PHARMA UK LIMITED
Reel/Frame 067652/0316 →
CHANGE OF ADDRESS Recorded Mar 21, 2019
From: HEPTARES THERAPEUTICS LIMITED
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 048661/0096 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2019
From: CUMMING, JOHN GRAHAM; WU, FRANK XINHE; EDMAN, KARL HENRIK; CHEN, HONGMING; BROWN, DEAN GORDON; BURLI, ROLAND WERNER; JOHNSTONE, SHAWN DONALD; BROWN, GILES ALBERT; TEHAN, BENJAMIN GERALD; TEOBALD, BARRY JOHN; CONGREVE, MILES STUART
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 048563/0120 →
Continuity (2)
Provisional Application 62335496 · May 12, 2016
Related Publication 20190144394A1 · May 16, 2019